Blood cholesterol is an important characteristic of lipid metabolism. Cholesterol-lowering therapy provided for patients with atherosclerosis and coronary heart disease results in a reduction of the cardiovascular death rate by 30-40%. There is a direct relationship between blood cholesterol levels and coronary diseases.
Cholesterol-lowering drugs are known which are based on plant preparations. In particular, a cholesterol-lowering drug (see RF Patent No. 2162333 according to IPC A61K35/78, published on Jan. 27, 2001) is known, which contains Licopodium (wolfs-claws), Aurum iodatum (auric iodate), Barium carbonicum (barium carbonate), Alluim sativum (garlic) taken in equal proportions at CI2 dilution. This drug is a mix of homeopathic preparations, each of these preparations being used for specific indications from arterial hypertension and atherosclerotic processes to chronic liver disease, urolithiasis, adiposity, etc. Use of a multicomponent drug like that described above is equivalent to polyprogmasy which usually makes patient's response to treatment difficult to interpret and ultimately precludes from making up an optimal treatment plan.
Another cholesterol-lowering drug based on plant preparation (see RF Patent No. 2152221 according to IPC A61K35/78, published on Jul. 10, 2000) is known which contains Salsola Collina herb dry extract as active substance.
Use of this plant preparation based on Salsola Collina is equivalent to the use of a combination of chemical substances because, as stated in the patent description, the active complex contains flavonoids, polysaccharides, carotinoids, sterines, saponins, lipids, amino acids and trace elements. As with above analogue, the variety like this is equivalent to polyprogmasy and will interfere with correct interpretation of patient's response to treatment. Furthermore, the content of active substance in the drug varies from 0.25 to 99.9% which is indicative of a low level of the drug standardization.
Other cholesterol-lowering drugs based on chemical preparations are known. Of particular interest are such drugs as nicotinic acid and its derivatives, bile acids sequestrants, fibric acid derivatives (fibrates), probucol (see Okorokov, A. N. Treatment of Internal Diseases/Practical Guide. Minsk: Vysheshaya Shkola, Vitebsk: Belmedkniga, 1996, vol. 3, book 1, pp. 19-41).
However, treatment with nicotinic acid is associated with a number of side effects, such as liver function impairment, exacerbation of chronic gastritis, gastric ulcer, and also can cause hyperglycemia, skin hyperemia and an elevation of blood levels of uric acid.
Therapy with sequestrants is associated with such side effects as nausea, flatulence, constipation and diarrhea. The treatment can also lead to elevation of triglycerides levels and impairment of digestion of fat-soluble vitamins (A, D, K) and folic acid.
Side effects of the use of fibrates (e.g. bezafibrate, fenophibrate, gemfibrozil) are muscle affection, an increase of lithiasis in biliary tracts, and a possibility to cause leucopenia, thrombocytopenia, and anemia.
Probucol favors ventricular arrythmias, dyspeptic disorders and can increase liver dysfunction.
Lovastatin (synonyms: Mevacor, Lovacor, Medostatin, Recol, Rovacol), a cholesterol-lowering drug, which regulates metabolic processes and contains an active substance of a chemical origin and special-purpose excipients, is the most closely related art drug to the claimed drug (see Vidal's Guide. Drugs in Russia. Moscow: AstraFarmServis, 2000, pp. B-364 to B-365).
The active substance of the related art drug belongs to statins and is [IS(I α (R*),3α,7β,8β(2S*,4S*),8αβ] 1,2,3,7,8 α, -Hexahydro-3,7-dimethyl-8[2-(tetrahydro)-4-hydroxy-6-oxo-2H-pyran-2-yl]-1-naphthalenyl 2-methyl butanoate. The substance acts by inhibiting cholesterol biosynthesis. In the body, lovastatin is metabolized to give β-oxyacid which is a competitive inhibitor of an enzyme 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase.
The related art drug also contains lactose, gelated starch, microcrystalline cellulose, butylated hydroxyanisol, indigotin (E132), and magnesium stearate as excipients.
A drawback of statins, including lovastatin, is that these drugs should be taken for long. Furthermore, statins can affect liver, muscles, gastrointestinal tract, cause sleep disturbances, headaches. In repeated drug administrations, the efficacy of the drug therapy can be reduced (tachyphylaxis) (see Cromwell W. C. Ziajka P. E. Development of tachyphylaxis among patients taking HMG CoA reductase inhibitors./Am J. Cardiol 2000; 86: 1123-1127// The translation is published in CONSILIUM medicum journal, 2001, vol. 3, no. 2. Translated by Elagin, R. I. Razvitie takhifilaksii u patsientov, poluchayushchikh ingibitory HMG-CoA reductasy). In addition, statins show xenobiotic properties.